JP2020508338A5 - - Google Patents
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- Publication number
- JP2020508338A5 JP2020508338A5 JP2019546286A JP2019546286A JP2020508338A5 JP 2020508338 A5 JP2020508338 A5 JP 2020508338A5 JP 2019546286 A JP2019546286 A JP 2019546286A JP 2019546286 A JP2019546286 A JP 2019546286A JP 2020508338 A5 JP2020508338 A5 JP 2020508338A5
- Authority
- JP
- Japan
- Prior art keywords
- bromo
- pyrimidine
- pharmaceutical composition
- compound
- yloxy
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 239000008194 pharmaceutical composition Substances 0.000 claims 17
- 150000001875 compounds Chemical class 0.000 claims 14
- 238000000634 powder X-ray diffraction Methods 0.000 claims 10
- 238000010586 diagram Methods 0.000 claims 9
- 125000004800 4-bromophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Br 0.000 claims 7
- 239000003814 drug Substances 0.000 claims 6
- DKULOVKANLVDEA-UHFFFAOYSA-N ACT-132577 Chemical compound C=1C=C(Br)C=CC=1C=1C(NS(=O)(=O)N)=NC=NC=1OCCOC1=NC=C(Br)C=N1 DKULOVKANLVDEA-UHFFFAOYSA-N 0.000 claims 5
- NVBFHJWHLNUMCV-UHFFFAOYSA-N Sulfamide Chemical compound NS(N)(=O)=O NVBFHJWHLNUMCV-UHFFFAOYSA-N 0.000 claims 5
- 229940079593 drugs Drugs 0.000 claims 5
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims 4
- 239000007787 solid Substances 0.000 claims 4
- 206010020772 Hypertension Diseases 0.000 claims 3
- 239000004480 active ingredient Substances 0.000 claims 3
- -1 pyrimidin-2-yloxy Chemical group 0.000 claims 3
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims 2
- GUBGYTABKSRVRQ-UUNJERMWSA-N Lactose Natural products O([C@@H]1[C@H](O)[C@H](O)[C@H](O)O[C@@H]1CO)[C@H]1[C@@H](O)[C@@H](O)[C@H](O)[C@H](CO)O1 GUBGYTABKSRVRQ-UUNJERMWSA-N 0.000 claims 2
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims 2
- XAPRFLSJBSXESP-UHFFFAOYSA-N Oxycinchophen Chemical compound N=1C2=CC=CC=C2C(C(=O)O)=C(O)C=1C1=CC=CC=C1 XAPRFLSJBSXESP-UHFFFAOYSA-N 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 claims 2
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims 2
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims 2
- 239000008101 lactose Substances 0.000 claims 2
- GUBGYTABKSRVRQ-XLOQQCSPSA-N lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 claims 2
- 235000019359 magnesium stearate Nutrition 0.000 claims 2
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims 2
- 239000008108 microcrystalline cellulose Substances 0.000 claims 2
- 229940016286 microcrystalline cellulose Drugs 0.000 claims 2
- 229960001681 Croscarmellose Sodium Drugs 0.000 claims 1
- 229920002785 Croscarmellose sodium Polymers 0.000 claims 1
- 239000002552 dosage form Substances 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 241000894007 species Species 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 0 Cc(cn1)cnc1OCCOc1ncnc(N*(N)=C)c1-c(cc1)ccc1Br Chemical compound Cc(cn1)cnc1OCCOc1ncnc(N*(N)=C)c1-c(cc1)ccc1Br 0.000 description 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2022201112A JP2023027305A (ja) | 2017-02-27 | 2022-12-16 | ４－ピリミジンスルファミド誘導体の結晶形 |
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP2017054489 | 2017-02-27 | ||
| EPPCT/EP2017/054489 | 2017-02-27 | ||
| EPPCT/EP2017/061487 | 2017-05-12 | ||
| EP2017061487 | 2017-05-12 | ||
| PCT/EP2018/054627 WO2018154101A1 (en) | 2017-02-27 | 2018-02-26 | Crystalline forms of the 4-pyrimidinesulfamide derivative aprocitentan |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022201112A Division JP2023027305A (ja) | 2017-02-27 | 2022-12-16 | ４－ピリミジンスルファミド誘導体の結晶形 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2020508338A JP2020508338A (ja) | 2020-03-19 |
| JP2020508338A5 true JP2020508338A5 (ko) | 2021-04-15 |
Family
ID=60268369
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019546291A Active JP7223701B2 (ja) | 2017-02-27 | 2017-11-06 | ４－ピリミジンスルファミド誘導体の、エンドセリン関連疾患治療用の有効成分との合剤 |
| JP2019546286A Pending JP2020508338A (ja) | 2017-02-27 | 2018-02-26 | ４−ピリミジンスルファミド誘導体の結晶形 |
| JP2022201112A Pending JP2023027305A (ja) | 2017-02-27 | 2022-12-16 | ４－ピリミジンスルファミド誘導体の結晶形 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019546291A Active JP7223701B2 (ja) | 2017-02-27 | 2017-11-06 | ４－ピリミジンスルファミド誘導体の、エンドセリン関連疾患治療用の有効成分との合剤 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022201112A Pending JP2023027305A (ja) | 2017-02-27 | 2022-12-16 | ４－ピリミジンスルファミド誘導体の結晶形 |
Country Status (17)
| Country | Link |
|---|---|
| US (5) | US11174247B2 (ko) |
| EP (3) | EP3658140A1 (ko) |
| JP (3) | JP7223701B2 (ko) |
| KR (3) | KR102568472B1 (ko) |
| CN (3) | CN110325186A (ko) |
| AU (2) | AU2017400276B2 (ko) |
| BR (2) | BR112019017658A2 (ko) |
| CA (2) | CA3053991A1 (ko) |
| CL (3) | CL2019002470A1 (ko) |
| IL (3) | IL297993A (ko) |
| MA (2) | MA49664A (ko) |
| MX (3) | MX2019010222A (ko) |
| PH (2) | PH12019501937A1 (ko) |
| SG (3) | SG11201907435PA (ko) |
| TW (2) | TW202330502A (ko) |
| UA (1) | UA126122C2 (ko) |
| WO (2) | WO2018153513A1 (ko) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110325186A (zh) * | 2017-02-27 | 2019-10-11 | 爱杜西亚药品有限公司 | 用于治疗内皮素相关疾病的4-嘧啶磺酰胺衍生物与活性成分的组合 |
| US20210169881A1 (en) * | 2017-11-30 | 2021-06-10 | Idorsia Pharmaceuticals Ltd | Combination of a 4-pyrimidinesulfamide derivative with an sglt-2 inhibitor for the treatment of endothelin related diseases |
| MA54522A (fr) | 2018-12-21 | 2022-03-23 | Actelion Pharmaceuticals Ltd | Composition pharmaceutique pour le traitement de l'hypertension artérielle pulmonaire |
| TW202042818A (zh) | 2019-01-25 | 2020-12-01 | 瑞士商艾克泰聯製藥有限公司 | 用於治療慢性血栓性肺高血壓之醫藥組成物 |
| CN112569357B (zh) * | 2019-09-30 | 2023-03-28 | 深圳奥萨制药有限公司 | 双重内皮素受体拮抗剂与利尿剂的组合物 |
| CN112679441A (zh) * | 2019-10-18 | 2021-04-20 | 普济生物科技（台州）有限公司 | 阿普昔腾坦的晶型、制备方法及其用途 |
| EP4056182A1 (en) * | 2019-11-07 | 2022-09-14 | Crystal Pharmaceutical (Suzhou) Co., Ltd. | Crystal form of aprocitentan, preparation method therefor and use thereof |
| EP4153574A1 (en) | 2020-05-21 | 2023-03-29 | Teva Pharmaceuticals International GmbH | Solid state forms of aprocitentan and process for preparation thereof |
| BR112023000406A2 (pt) | 2020-07-10 | 2023-01-31 | Astrazeneca Ab | Combinação de zibotentan e dapagliflozina |
| WO2023111797A1 (en) * | 2021-12-17 | 2023-06-22 | Janssen Biotech, Inc. | Pyrimidine sulfamide derivatives and process for manufacturing them |
| WO2023227490A1 (en) | 2022-05-22 | 2023-11-30 | Idorsia Pharmaceuticals Ltd | Aprocitentan for the treatment of hypertension |
| WO2023227721A1 (en) | 2022-05-25 | 2023-11-30 | Idorsia Pharmaceuticals Ltd | Crystalline forms of sodium (5-(4-bromophenyl)-6-(2-((5-bromopyrimidin-2-yl)oxy)ethoxy)pyrimidin-4-yl)(sulfamoyl)amide |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE59409631D1 (de) * | 1993-07-15 | 2001-02-15 | Hoffmann La Roche | Pharmazeutische Kombination, die einen Hemmer des Renin-Angiotensin-Systems und einen Endothelin-Antagonisten enthält |
| EP1345920B1 (en) | 2000-12-18 | 2006-04-12 | Actelion Pharmaceuticals Ltd. | Novel sulfamides and their use as endothelin receptor antagonists |
| EG24716A (en) | 2002-05-17 | 2010-06-07 | Novartis Ag | Combination of organic compounds |
| US20070196510A1 (en) | 2006-02-17 | 2007-08-23 | Gerber Michael J | Method for treating resistant hypertension |
| CA2655144A1 (en) | 2006-06-15 | 2007-12-21 | Gilead Colorado, Inc. | Antihypertensive therapy method |
| AR061627A1 (es) | 2006-06-27 | 2008-09-10 | Novartis Ag | Formas de dosificacion solidas de valsartan, amlodipina, e hidroclorotiazida, y metodo para elaborarlas |
| MX2010001837A (es) * | 2007-08-17 | 2010-03-10 | Actelion Pharmaceuticals Ltd | Derivados de 4-pirimidinasulfamida. |
| US20090054473A1 (en) | 2007-08-22 | 2009-02-26 | Gilead Colorado, Inc. | Therapy for complications of diabetes |
| CN102614189B (zh) * | 2012-04-17 | 2014-10-22 | 北京哈三联科技股份有限公司 | 含缬沙坦、氨氯地平和氢氯噻嗪的微丸药物组合 |
| EP2907811A1 (en) * | 2014-02-14 | 2015-08-19 | Actelion Pharmaceuticals Ltd. | Process for manufacturing pyrimidine sulfamide derivatives |
| AU2015342929A1 (en) | 2014-11-07 | 2017-05-25 | Abbvie Inc. | Methods of treating CKD using predictors of fluid retention |
| WO2017185142A1 (en) | 2016-04-29 | 2017-11-02 | Adelaide Research & Innovation Pty Ltd | Method for preventing and/or treating atrial fibrillation |
| CN110325186A (zh) | 2017-02-27 | 2019-10-11 | 爱杜西亚药品有限公司 | 用于治疗内皮素相关疾病的4-嘧啶磺酰胺衍生物与活性成分的组合 |
| US20210169881A1 (en) | 2017-11-30 | 2021-06-10 | Idorsia Pharmaceuticals Ltd | Combination of a 4-pyrimidinesulfamide derivative with an sglt-2 inhibitor for the treatment of endothelin related diseases |
| MA54522A (fr) * | 2018-12-21 | 2022-03-23 | Actelion Pharmaceuticals Ltd | Composition pharmaceutique pour le traitement de l'hypertension artérielle pulmonaire |
-
2017
- 2017-11-06 CN CN201780087445.XA patent/CN110325186A/zh active Pending
- 2017-11-06 MA MA049664A patent/MA49664A/fr unknown
- 2017-11-06 JP JP2019546291A patent/JP7223701B2/ja active Active
- 2017-11-06 AU AU2017400276A patent/AU2017400276B2/en active Active
- 2017-11-06 KR KR1020197028199A patent/KR102568472B1/ko active IP Right Grant
- 2017-11-06 WO PCT/EP2017/078371 patent/WO2018153513A1/en active Application Filing
- 2017-11-06 BR BR112019017658-6A patent/BR112019017658A2/pt unknown
- 2017-11-06 EP EP17794712.4A patent/EP3658140A1/en active Pending
- 2017-11-06 US US16/489,227 patent/US11174247B2/en active Active
- 2017-11-06 SG SG11201907435PA patent/SG11201907435PA/en unknown
- 2017-11-06 CA CA3053991A patent/CA3053991A1/en active Pending
- 2017-11-06 KR KR1020237016438A patent/KR20230074610A/ko not_active Application Discontinuation
- 2017-11-06 MX MX2019010222A patent/MX2019010222A/es unknown
- 2017-11-06 UA UAA201909965A patent/UA126122C2/uk unknown
-
2018
- 2018-02-26 JP JP2019546286A patent/JP2020508338A/ja active Pending
- 2018-02-26 SG SG11201907604UA patent/SG11201907604UA/en unknown
- 2018-02-26 CN CN201880014146.8A patent/CN110381948A/zh active Pending
- 2018-02-26 SG SG10202111695RA patent/SG10202111695RA/en unknown
- 2018-02-26 EP EP18708945.3A patent/EP3585391A1/en not_active Withdrawn
- 2018-02-26 CA CA3053994A patent/CA3053994A1/en active Pending
- 2018-02-26 TW TW111142832A patent/TW202330502A/zh unknown
- 2018-02-26 AU AU2018225309A patent/AU2018225309B2/en active Active
- 2018-02-26 IL IL297993A patent/IL297993A/en unknown
- 2018-02-26 TW TW107106403A patent/TWI786089B/zh active
- 2018-02-26 MA MA047596A patent/MA47596A/fr unknown
- 2018-02-26 WO PCT/EP2018/054627 patent/WO2018154101A1/en active Application Filing
- 2018-02-26 EP EP21202979.7A patent/EP4014976A1/en active Pending
- 2018-02-26 MX MX2019010221A patent/MX2019010221A/es unknown
- 2018-02-26 BR BR112019017644-6A patent/BR112019017644A2/pt unknown
- 2018-02-26 KR KR1020197028200A patent/KR102577375B1/ko active IP Right Grant
- 2018-02-26 CN CN202311718027.XA patent/CN117946011A/zh active Pending
- 2018-02-26 US US16/489,194 patent/US10919881B2/en active Active
-
2019
- 2019-08-22 IL IL26885019A patent/IL268850A/en unknown
- 2019-08-22 PH PH12019501937A patent/PH12019501937A1/en unknown
- 2019-08-22 PH PH12019501938A patent/PH12019501938A1/en unknown
- 2019-08-22 IL IL26885219A patent/IL268852A/en unknown
- 2019-08-27 CL CL2019002470A patent/CL2019002470A1/es unknown
- 2019-08-27 CL CL2019002464A patent/CL2019002464A1/es unknown
- 2019-08-27 MX MX2021007184A patent/MX2021007184A/es unknown
-
2020
- 2020-06-30 CL CL2020001762A patent/CL2020001762A1/es unknown
-
2021
- 2021-01-12 US US17/146,801 patent/US11680058B2/en active Active
- 2021-09-10 US US17/472,349 patent/US11787782B2/en active Active
-
2022
- 2022-12-16 JP JP2022201112A patent/JP2023027305A/ja active Pending
-
2023
- 2023-05-17 US US18/319,402 patent/US20230391757A1/en active Pending
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